885499-61-6

Basic information

• Product Name: CCT128930
• Synonyms: 4-(4-chlorobenzyl)-1-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidin-4-aMine;4-[(4-Chlorophenyl)methyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinamine;4-PiperidinaMine, 4-[(4-chlorophenyl)Methyl]-1-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-;CCT128930, >=98%
• CAS NO: 885499-61-6
• Molecular Formula: C₁₈H₂₀ClN₅
• Molecular Weight: 341.8379
• Product Categories: Inhibitors;Akt;mTOR;PI3K
• Mol File: 885499-61-6.mol
• Article Data: 5

Chemical Properties

• Boiling Point: 547.902 °C at 760 mmHg
• Flash Point: 285.161 °C
• Appearance: /
• Density: 1.39
• PKA: 13.93±0.50(Predicted)
• CAS DataBase Reference: CCT128930(CAS DataBase Reference)
• NIST Chemistry Reference: CCT128930(885499-61-6)
• EPA Substance Registry System: CCT128930(885499-61-6)

Safety Data

• Hazardous Substances Data: 885499-61-6(Hazardous Substances Data)

Usage

Description

CCT128930 is a potent, ATP-competitive, and selective inhibitor of Akt2, a protein kinase involved in various cellular processes, with an IC50 of 6 nM.

Uses

Used in Pharmaceutical Industry:
CCT128930 is used as a research tool for studying the role of Akt2 in cellular processes and as a potential therapeutic agent for treating diseases associated with Akt2 dysregulation.
Used in Cancer Research:
CCT128930 is used as a selective inhibitor of Akt2 for investigating its role in cancer cell survival, proliferation, and resistance to therapy. It may also be used in combination with other targeted therapies to enhance their efficacy in treating cancer.
Used in Drug Discovery:
CCT128930 serves as a lead compound for the development of novel Akt2 inhibitors with improved potency, selectivity, and pharmacokinetic properties, which can be used in the treatment of various diseases, including cancer and metabolic disorders.

Upstream product

• 885500-38-9 4-(4-chlorobenzyl)piperidin-4-ylamine dihydrochloride 
• 3680-69-1 4-chloro-1H-pyrrolo[2,3-d]pyrimidine 
• 170284-71-6 1-(tert-butoxycarbonyl)-4-(4-chlorobenzyl)piperidine-4-carboxylic acid 
• 885653-43-0 4-(4-chlorobenzyl)-piperidin-4-ylamine 
• 956460-41-6 C₁₇H₂₅ClN₂O₂ 
• 885500-37-8 4-(4-chlorobenzyl)piperidine-1,4-dicarboxylic acid 1-tert-butyl ester 4-methyl ester 
• 100-39-0 benzyl bromide 
• 104-83-6 1-Chloro-4-(chloromethyl)benzene 
• 3680-71-5 Allopurinol 
• 741687-09-2 tert-butyl 4-amino-4-benzylpiperidine-1-carboxylate 
• 167263-11-8 N-tert-butyloxycarbonyl-4-benzylpiperidine-4-carboxylic acid 
• 741687-06-9 1-tert-butyl 4-methyl 4-benzylpiperidine-1,4-dicarboxylate 
• 887129-20-6 C₂₂H₃₃ClN₂O₄ 

Relevant articles and documents

Discovery of 4-amino-l-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4- carboxamides as selective, orally active inhibitors of protein kinase B (Akt)

Protein kinase B (PKB or Akt) is an important component of intracellular signaling pathways regulating growth and survival. Signaling through PKB is frequently deregulated in cancer, and inhibitors of PKB therefore have potential as antitumor agents. The optimization of lipophilic substitution within a series of 4-benzyl-l-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amines provided ATP-competitive, nanomolar inhibitors with up to 150-fold selectivity for inhibition of PKB over the closely related kinase PKA. Although active in cellular assays, compounds containing 4-amino-4-benzylpiperidines underwent metabolism in vivo, leading to rapid clearance and low oral bioavailability. Variation of the linker group between the piperidine and the lipophilic substituent identified 4-amino-l-(7H-pyrrolo[2,3-d]-pyrimidin-4-yl)piperidine-4- carboxamides as potent and orally bioavailable inhibitors of PKB. Representative compounds modulated biomarkers of signaling through PKB in vivo and strongly inhibited the growth of human tumor xenografts in nude mice at well-tolerated doses.

PHARMACEUTICAL COMPOUNDS

The invention provides compounds of the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein J1-J2 is CH=CH, N=CH, CH=N, HN-C(O) or CH2CO; T is N or CH and GP is as defined in the claims. The compounds have activity as inhibitors of PKA and PKB kinases and are useful in the treatment of cancers.

ORTHO-CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E.G. PURINES) AS PROTEIN KINASES INHIBITORS

-